公开(公告)号：US20140155418A1

公开(公告)日：2014-06-05

申请号：US14060123

申请日：2013-10-22

申请人： SYMPHONY EVOLUTION, INC.

发明人： Kenneth D. Rice ,  Neel K. Anand ,  Joerg Bussenius ,  Simona Costanzo ,  Abigail R. Kennedy ,  Csaba J. Peto ,  Tsze H. Tsang ,  Charles M. Blazey

IPC分类号： C07D403/12

CPC分类号： C07D403/12 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5513 ,  A61K31/553 ,  A61K31/7064 ,  C07D239/94 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04

摘要： The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.

摘要翻译： 本发明提供用于调节受体激酶活性的化合物，特别是ephrin和EGFR，以及利用其化合物及其药物组合物治疗由受体激酶活性介导的疾病的方法。 由受体激酶活性介导的疾病包括但不限于由细胞增殖异常水平（即肿瘤生长），程序性细胞死亡（细胞凋亡），细胞迁移和与肿瘤生长相关的血管生成的特征的疾病。 本发明的化合物包括“光谱选择性”激酶调节剂，抑制，调节和/或调节受体型酪氨酸激酶（包括ephrin和EGFR）亚家族的信号转导的化合物。

公开(公告)号：US09163006B2

公开(公告)日：2015-10-20

申请号：US14060123

申请日：2013-10-22

申请人： Symphony Evolution, Inc.

发明人： Kenneth D. Rice ,  Neel K. Anand ,  Joerg Bussenius ,  Simona Costanzo ,  Abigail R. Kennedy ,  Csaba J. Peto ,  Tsze H. Tsang ,  Charles M. Blazey

IPC分类号： C07D209/52 ,  C07D239/94 ,  C07D403/12 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04

摘要： The present disclosure provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. The compounds are generally of formula (I): Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.Also disclosed are methods of making compounds for formula 8: comprising introducing group E2 into a compound of formula 7: wherein Ar, Z, P, and E2 are defined herein.

公开(公告)号：US10266518B2

公开(公告)日：2019-04-23

申请号：US15692445

申请日：2017-08-31

申请人： Symphony Evolution, Inc.

发明人： Kenneth D. Rice ,  Neel K. Anand ,  Joerg Bussenius ,  Simona Costanzo ,  Abigail R. Kennedy ,  Csaba J. Peto ,  Tsze H. Tsang ,  Charles M. Blazey

IPC分类号： A61K31/517 ,  C07D239/94 ,  C07D403/12 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5513 ,  A61K31/553 ,  A61K31/7064

摘要： The present invention provides compounds of Formula I, for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.

公开(公告)号：US09796704B2

公开(公告)日：2017-10-24

申请号：US14845763

申请日：2015-09-04

申请人： Symphony Evolution, Inc.

发明人： Kenneth D. Rice ,  Neel K. Anand ,  Joerg Bussenius ,  Simona Costanzo ,  Abigail R. Kennedy ,  Csaba J. Peto ,  Tsze H. Tsang ,  Charles M. Blazey

IPC分类号： C07D239/94 ,  C07D403/12 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5513 ,  A61K31/553 ,  A61K31/7064

CPC分类号： C07D403/12 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5513 ,  A61K31/553 ,  A61K31/7064 ,  C07D239/94 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04

摘要： The present invention provides compounds of structural formula I, for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.

公开(公告)号：US09359332B2

公开(公告)日：2016-06-07

申请号：US14060123

申请日：2013-10-22

申请人： Symphony Evolution, Inc.

发明人： Kenneth D. Rice ,  Neel K. Anand ,  Joerg Bussenius ,  Simona Costanzo ,  Abigail R. Kennedy ,  Csaba J. Peto ,  Tsze H. Tsang ,  Charles M. Blazey

IPC分类号： C07D209/52 ,  C07D239/94 ,  C07D403/12 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04

CPC分类号： C07D403/12 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5513 ,  A61K31/553 ,  A61K31/7064 ,  C07D239/94 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04

摘要： The present disclosure provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. The compounds are generally of formula (I): Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.Also disclosed are methods of making compounds for formula 8: comprising introducing group E2 into a compound of formula 7: wherein Ar, Z, P, and E2 are defined herein.

摘要翻译： 本公开提供了用于调节受体激酶活性的化合物，特别是ephrin和EGFR，以及利用其化合物及其药物组合物治疗由受体激酶活性介导的疾病的方法。 化合物通常为式（I）：由受体激酶活性介导的疾病包括但不限于以部分由细胞增殖异常水平（即肿瘤生长），程序性细胞死亡（细胞凋亡），细胞迁移和 与肿瘤生长相关的侵袭和血管生成。 本发明的化合物包括“光谱选择性”激酶调节剂，抑制，调节和/或调节受体型酪氨酸激酶（包括ephrin和EGFR）亚家族的信号转导的化合物。 还公开了制备式8化合物的方法：包括将E2组导入式7化合物中：其中Ar，Z，P和E2在本文中定义。

公开(公告)号：US20180118724A1

公开(公告)日：2018-05-03

申请号：US15692445

申请日：2018-01-15

申请人： Symphony Evolution, Inc.

发明人： Kenneth D. Rice ,  Neel K. Anand ,  Joerg Bussenius ,  Simona Costanzo ,  Abigail R. Kennedy ,  Csaba J. Peto ,  Tsze H. Tsang ,  Charles M. Blazey

IPC分类号： C07D403/12 ,  A61K31/517 ,  C07D487/04 ,  C07D493/04 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/553 ,  A61K31/5513 ,  A61K31/7064 ,  C07D239/94 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/04

CPC分类号： C07D403/12 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5513 ,  A61K31/553 ,  A61K31/7064 ,  C07D239/94 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04

摘要： The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.